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GM 6001 Sale

(Synonyms: 伊洛马司他; GM6001; Galardin) 目录号 : GC14523

A broad spectrum inhibitor of zinc-containing proteases

GM 6001 Chemical Structure

Cas No.:142880-36-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,313.00
现货
5mg
¥746.00
现货
10 mg
¥1,061.00
现货
50mg
¥3,297.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

MDA-MB-435 cells

Preparation method

Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

1, 2, 4 nM; 6 or 12 h.

Applications

In MDA-MB-435 cells, GM 6001 increases the respiratory rate by 80% and [3H] thymidine incorporation by 50% when treated for 6 h and 12 h respectively, which suggest that GM 6001 increase DNA synthesis. GM 6001 also increases ERK activity and p38 kinase activity.

Animal experiment [2]:

Animal models

Rats with balloon injury of the carotid artery.

Dosage form

100 mg/kg; 2, 4, 7, 10, or 14 days; IP injection.

Preparation method

Dissolved in 4% CMC.

Applications

GM 6001 reduces the amount of SMCs that migrated into the intima by 97% at 4 days after injury and inhibits lesions growth, which is mediated by MMP. However, at 14 days after injury, intimal area and the amount of SMCs were the same in GM 6001-treated and control rats.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Porter JF, Shen S, Denhardt DT. Tissue inhibitor of metalloproteinase-1 stimulates proliferation of human cancer cells by inhibiting a metalloproteinase. Br J Cancer, 2004, 90(2): 463-470.

[2]. Bendeck MP, Irvin C, Reidy MA. Inhibition of matrix metalloproteinase activity inhibits smooth muscle cell migration but not neointimal thickening after arterial injury. Circ Res, 1996, 78(1): 38-43.

产品描述

GM 6001 is a broad-spectrum inhibitor of MMP with Ki values of 0.4nM, 0.5nM, 27nM, 0.1nM and 0.2nM, respectively for MMP-1,2,3,8 and 9 [1].

MMPs are divided into 4 subfamilies: stromelysins, gelatinases, membrane-type MMPs, and collagenases. They play major roles in mediating the effects of IL-1 during meniscal healing. As an inhibitor of MMP, GM 6001 is reported to enhance the repair of meniscal lesions in an inflammatory microenvironment. MMPs also play roles in the transactivation of EGFR induced by GPCR agonists. It is reported that treatment of GM 6001 inhibits the phosphorylation of EGFR as well as the activation of ERK induced by bombesin or LPA. The DNA synthesis induced by bombesin or LPA is also attenuated by GM 6001 since the activity of MMP is required for the GPCR-induced late response mitogenic signaling [1, 2].

References:
[1] McNulty AL, Weinberg JB, Guilak F. Inhibition of matrix metalloproteinases enhances in vitro repair of the meniscus. Clin Orthop Relat Res. 2009 Jun;467(6):1557-67.
[2] Santiskulvong C, Rozengurt E. Galardin (GM 6001), a broad-spectrum matrix metalloproteinase inhibitor, blocks bombesin- and LPA-induced EGF receptor transactivation and DNA synthesis in rat-1 cells. Exp Cell Res. 2003 Nov 1;290(2):437-46.

Chemical Properties

Cas No. 142880-36-2 SDF
别名 伊洛马司他; GM6001; Galardin
化学名 (2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide
Canonical SMILES CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC
分子式 C20H28N4O4 分子量 388.46
溶解度 ≥ 19.423 mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.5743 mL 12.8713 mL 25.7427 mL
5 mM 0.5149 mL 2.5743 mL 5.1485 mL
10 mM 0.2574 mL 1.2871 mL 2.5743 mL
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